MLCK

抑制剂选择性比较

MLCK产品

所有产品 MLCK抑制剂(4) MLCK调节剂(1)

目录号	产品描述	文献引用	实验数据
S1573	Fasudil (HA-1077) HCl Fasudil(HA-1077)是一种有效的、具有选择性的Rho抑制剂（ROCK2, Ki=0.33 μM），同时对PKA、PKG、PKC和MLCK也具有抑制活性，Ki值分别为1.6 μM、1.6 μM、3.3 μM、36 μM。Fasudil 也是calcium channel的阻滞剂。	Nat Cell Biol, 2020, 25 Nat Commun, 2020, 11(1):71 Cell Rep, 2020, 30(11):3864-3874	The ROCK inhibitors fasudil and Y27632 prevented SCP2 cell bone metastasis in nude mice (n = 10 per group). Shown are BLI images of bone metastases, IHC analyses of SMAD3 C-tail phosphorylation and PTHLH, osteoclast TRAP staining, and BLI quantitation.
S7099	(-)-Blebbistatin (-)-Blebbistatin是一种细胞渗透性抑制剂，作用于非肌球蛋白IIATPase，无细胞试验中IC50为~2 μM，不抑制肌球蛋白轻链激酶，抑制卵裂沟的缢缩，不干扰有丝分裂或收缩环的组装。	Nat Cell Biol, 2020, 25 Cell Rep, 2020, 30(11):3864-3874 Cell Death Dis, 2020, 8;11(6):428	(C) MyoIIA inhibition by blebbistatin treatment in vivo impairs leukemia cell extravasation into the brain. One hour before B-ALL cell transfer, C57BL/6 CD45.1+ recipient mice were treated with vehicle or blebbistatin (2.5 mg/kg). Twenty-four hours after B-ALL cell transfer, the recipient mice were intravenously injected with CD19-APC antibodies and then euthanized 4 min later.
S8388	ML-7 HCl ML-7 是平滑肌肌球蛋白轻链激酶MLCK抑制剂，Ki值为0.3 μM。对钙离子-钙调蛋白依赖性或非依赖性的平滑肌MLCKs具有可逆的、ATP竞争性抑制作用。ML-7 还可抑制 PKA 和 PKC，对应的Ki值分别为21 μM和42 μM。	Cancer Lett, 2020, 28;483:75-86 Stem Cells, 2020, 11 Exp Cell Res, 2018, 363(2):321-331	Platelets (3 × 10⁸/mL) were treated with ML-7 (5 µM) for 20 minutes, followed by stimulation with oxLDL (50 µg/mL) for 15 seconds. Samples were then lysed, separated by SDS-PAGE, and immunoblotted for phospho-MLCSer19 followed by reprobing for β-tubulin. (Ai) Representative blots. (Aii) Densitometric analysis of 5 independent experiments. *P < .05.
S6847^New	ML-9 HCl ML-9 HCl (ML-9 hydrochloride) 是一种有效的选择性的 Akt kinase、myosin light chain kinase (MLCK) 和 stromal interaction molecule 1 (STIM1)。ML-9 HCl 也是 Ca2+-permeable channels 的有效抑制剂。ML-9 HCl 是一种靶向自噬和细胞死亡的亲溶酶体剂。
S8861^New	Mavacamten (MYK-461) Mavacamten (MYK-461)是心肌肌球蛋白（cardiac myosin）的小分子调节剂，调节肥厚型心肌病的肌节过强收缩。

目录号	产品描述	文献引用	实验数据
S1573	Fasudil (HA-1077) HCl Fasudil(HA-1077)是一种有效的、具有选择性的Rho抑制剂（ROCK2, Ki=0.33 μM），同时对PKA、PKG、PKC和MLCK也具有抑制活性，Ki值分别为1.6 μM、1.6 μM、3.3 μM、36 μM。Fasudil 也是calcium channel的阻滞剂。	Nat Cell Biol,2020, 25 Nat Commun,2020, 11(1):71 Cell Rep,2020, 30(11):3864-3874	The ROCK inhibitors fasudil and Y27632 prevented SCP2 cell bone metastasis in nude mice (n = 10 per group). Shown are BLI images of bone metastases, IHC analyses of SMAD3 C-tail phosphorylation and PTHLH, osteoclast TRAP staining, and BLI quantitation.
S7099	(-)-Blebbistatin (-)-Blebbistatin是一种细胞渗透性抑制剂，作用于非肌球蛋白IIATPase，无细胞试验中IC50为~2 μM，不抑制肌球蛋白轻链激酶，抑制卵裂沟的缢缩，不干扰有丝分裂或收缩环的组装。	Nat Cell Biol,2020, 25 Cell Rep,2020, 30(11):3864-3874 Cell Death Dis,2020, 8;11(6):428	(C) MyoIIA inhibition by blebbistatin treatment in vivo impairs leukemia cell extravasation into the brain. One hour before B-ALL cell transfer, C57BL/6 CD45.1+ recipient mice were treated with vehicle or blebbistatin (2.5 mg/kg). Twenty-four hours after B-ALL cell transfer, the recipient mice were intravenously injected with CD19-APC antibodies and then euthanized 4 min later.
S8388	ML-7 HCl ML-7 是平滑肌肌球蛋白轻链激酶MLCK抑制剂，Ki值为0.3 μM。对钙离子-钙调蛋白依赖性或非依赖性的平滑肌MLCKs具有可逆的、ATP竞争性抑制作用。ML-7 还可抑制 PKA 和 PKC，对应的Ki值分别为21 μM和42 μM。	Cancer Lett,2020, 28;483:75-86 Stem Cells,2020, 11 Exp Cell Res,2018, 363(2):321-331	Platelets (3 × 10⁸/mL) were treated with ML-7 (5 µM) for 20 minutes, followed by stimulation with oxLDL (50 µg/mL) for 15 seconds. Samples were then lysed, separated by SDS-PAGE, and immunoblotted for phospho-MLCSer19 followed by reprobing for β-tubulin. (Ai) Representative blots. (Aii) Densitometric analysis of 5 independent experiments. *P < .05.
S6847^New	ML-9 HCl ML-9 HCl (ML-9 hydrochloride) 是一种有效的选择性的 Akt kinase、myosin light chain kinase (MLCK) 和 stromal interaction molecule 1 (STIM1)。ML-9 HCl 也是 Ca2+-permeable channels 的有效抑制剂。ML-9 HCl 是一种靶向自噬和细胞死亡的亲溶酶体剂。

目录号

产品描述

文献引用

实验数据

S8861^New

Mavacamten (MYK-461)

Mavacamten (MYK-461)是心肌肌球蛋白（cardiac myosin）的小分子调节剂，调节肥厚型心肌病的肌节过强收缩。